Usage
- Cefoperazone + Tazobactam is prescribed for a wide range of bacterial infections, including intra-abdominal infections, respiratory tract infections (pneumonia, bronchitis), skin and soft tissue infections, urinary tract infections, septicemia, and bacterial meningitis. It is particularly effective against Pseudomonas aeruginosa infections.
- Pharmacological Classification: Antibiotic, specifically a third-generation cephalosporin combined with a beta-lactamase inhibitor.
- Mechanism of Action: Cefoperazone inhibits bacterial cell wall synthesis, leading to bacterial cell death. Tazobactam inhibits beta-lactamase, an enzyme produced by some bacteria that can break down cefoperazone, thereby extending cefoperazone’s spectrum of activity.
Alternate Names
- Cefoperazone/Tazobactam
- Brand Names: Numerous brand names exist, including Magnex, Ceftum, Cefopar, and others, which may vary regionally.
How It Works
- Pharmacodynamics: Cefoperazone + Tazobactam exerts bactericidal activity by disrupting bacterial cell wall synthesis. Tazobactam enhances cefoperazone’s effectiveness by inhibiting beta-lactamase enzymes produced by certain bacteria. It is particularly effective against gram-negative bacteria, including Pseudomonas aeruginosa.
- Pharmacokinetics: Administered intravenously (IV) or intramuscularly (IM). Cefoperazone achieves peak plasma concentrations within 1 to 2 hours after IM administration. Tazobactam exhibits nonlinear, dose-dependent pharmacokinetics. Cefoperazone is excreted primarily in bile, while tazobactam is eliminated mainly through renal excretion. Cefoperazone’s half-life is approximately 2 hours.
- Mode of Action: Cefoperazone binds to penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall, inhibiting the final transpeptidation step of peptidoglycan synthesis. Tazobactam irreversibly binds to and inactivates beta-lactamases.
- Elimination Pathways: Cefoperazone is primarily excreted in bile, while tazobactam is predominantly excreted through the kidneys.
Dosage
Standard Dosage
Adults:
- The typical adult dose is 2 to 4 grams per day, administered in equally divided doses every 12 hours.
- For severe infections, higher doses (up to 12 g/day) may be used.
Children:
- Safety and efficacy have not been established in children younger than 12 years.
- Dosing in older children (≥12 years) may follow adult recommendations, adjusted for weight and renal function.
Special Cases:
- Elderly Patients: Monitor renal function; dosage adjustments may be necessary.
- Patients with Renal Impairment: Reduce the dose based on creatinine clearance.
- Patients with Hepatic Dysfunction: Caution is advised; dosage adjustments may be necessary.
- Patients with Comorbid Conditions: Individualized dosing may be required based on specific conditions.
Clinical Use Cases
- Intubation, Surgical Procedures, Mechanical Ventilation, ICU Use, Emergency Situations: Dosing should be based on infection severity and adjusted according to renal function. Standard adult doses are often appropriate, but higher doses may be necessary in severe infections.
Dosage Adjustments
- Dose modification is necessary for patients with renal or hepatic dysfunction, based on the degree of impairment.
Side Effects
Common Side Effects
- Diarrhea
- Nausea
- Vomiting
- Pain and inflammation at the injection site
- Rash
Rare but Serious Side Effects
- Severe allergic reactions (anaphylaxis)
- Pseudomembranous colitis (Clostridium difficile-associated diarrhea)
- Bleeding or bruising
- Jaundice
Long-Term Effects
- With prolonged use, some patients may develop vitamin K deficiency, increasing the risk of bleeding.
Adverse Drug Reactions (ADR)
- Severe hypersensitivity reactions, including anaphylaxis, Stevens-Johnson Syndrome and toxic epidermal necrolysis.
- Neutropenia (low white blood cell count)
- Hepatotoxicity (liver damage)
Contraindications
- Known hypersensitivity to cefoperazone, tazobactam, penicillins, or other cephalosporins.
Drug Interactions
- Alcohol (disulfiram-like reaction)
- Aminoglycosides (increased risk of nephrotoxicity)
- Anticoagulants (increased risk of bleeding)
- Probenecid (may increase cefoperazone levels)
Pregnancy and Breastfeeding
- Pregnancy Safety Category: There are no adequate and well-controlled studies in pregnant women; use only if clearly needed.
- Cefoperazone crosses the placenta, and low concentrations are found in breast milk. Use with caution during breastfeeding.
Drug Profile Summary
- Mechanism of Action: Inhibits bacterial cell wall synthesis (Cefoperazone) and beta-lactamase inhibitor (Tazobactam).
- Side Effects: Diarrhea, nausea, vomiting, injection site reactions, rash, allergic reactions.
- Contraindications: Hypersensitivity to cefoperazone, tazobactam, penicillins, or other cephalosporins.
- Drug Interactions: Alcohol, aminoglycosides, anticoagulants, probenecid.
- Pregnancy & Breastfeeding: Use with caution; no adequate studies in pregnant women.
- Dosage: 2-4g/day divided every 12 hours (adults); adjust for renal/hepatic impairment.
- Monitoring Parameters: Renal function, liver function tests, complete blood count, signs of allergic reaction.
Popular Combinations
- Often used as a single agent due to its broad spectrum.
Precautions
- General Precautions: Assess for history of allergies to beta-lactam antibiotics. Monitor renal and hepatic function.
- Specific Populations: Use cautiously in pregnant/breastfeeding women, elderly, and patients with renal/hepatic impairment.
- Lifestyle Considerations: Avoid alcohol during and for several days after treatment.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Cefoperazone + Tazobactum?
A: The usual adult dose is 2 to 4 g/day, given in equally divided doses every 12 hours IV or IM. Dosage adjustments are required for renal or hepatic impairment.
Q2: What infections is Cefoperazone + Tazobactam effective against?
A: It is indicated for a broad range of bacterial infections, including intra-abdominal, respiratory tract, skin and soft tissue, urinary tract, septicemia, and meningitis. It is particularly effective against Pseudomonas aeruginosa.
Q3: Can it be used in children?
A: Safety and efficacy haven’t been established in children under 12. Older children’s dosages should be adjusted based on weight and renal function.
Q4: Are there any major drug interactions?
A: Yes, avoid alcohol, aminoglycosides, anticoagulants, and probenecid due to potential interactions.
Q5: Can pregnant or breastfeeding women take it?
A: Use with caution. No adequate and controlled studies exist in pregnant women. Low drug concentrations are found in breast milk.
Q6: What are the most common side effects?
A: Common side effects include diarrhea, nausea, vomiting, and injection site reactions.
Q7: What should be monitored during treatment?
A: Monitor renal and hepatic function, complete blood count, and for signs of allergic reaction.
Q8: What should I do if a patient experiences an allergic reaction?
A: Discontinue the drug immediately and provide appropriate supportive care, such as epinephrine, antihistamines, and corticosteroids.
Q9: How is Cefoperazone + Tazobactam administered?
A: It is administered intravenously (IV) or intramuscularly (IM). IV infusions should be administered slowly over 15-30 minutes.
